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首页-小分子抑制剂&激动剂-Others-Other Targets-DH20931
DH20931

Chemical Structure : DH20931

CAS No.: 1629992-28-4

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DH20931 (DH-20931)

货号: PC-25458Not For Human Use, Lab Use Only.

DH20931 is a first-in-class, potent small-molecule agonist of Ceramide Synthase 2 (CerS2) with activation constant (Kact) of 16.54 nM, exhibits potent, broad-spectrum, and receptor-independent antitumor activity in vitro and in vivo.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DH20931 is a first-in-class, potent small-molecule agonist of Ceramide Synthase 2 (CerS2) with activation constant (Kact) of 16.54 nM, exhibits potent, broad-spectrum, and receptor-independent antitumor activity in vitro and in vivo.
DH20931 exhibits the significant growth inhibitory effects on both triple-positive and triple-negative human breast cancer cell lines with IC50 in the range of 0.3-3.9 uM.
DH20931 potently inhibits the viability of wild-type 4T1 cells, but CERS2-knockout cells.
DH20931 exerts its cytotoxic effects by directly activating CerS2 and driving the overproduction of pro-apoptotic VLCCs.
DH20931 inhibits breast cancer growth in vitro and in vivo, independent of hormone receptor status.
DH20931 induces ER stress through the ATF4 pathway in a CerS2-dependent manner.
DH20931 promotes a novel CerS2-IP3R1 interaction, enhances ER-mitochondria proximity, and triggers mitochondrial Ca²⁺ overload.
DH20931 induces robust apoptosis in breast cancer cells in a CerS2-dependent manner.

物理化学性质&存储条件

分子量 368.86
分子式 C21H21ClN2O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

3,13-dimethoxy-5,6,10,11-tetrahydroimidazo[4,3-a:5,1-a']diisoquinolin-7-ium chloride

参考文献

1. Zajac-Kaye M, et al. bioRxiv [Preprint]. 2025 Aug 21:2025.08.15.670525.

2. Jaiswal AS, et al. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4850-3.

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